Canertinib dihydrochloride 是一种可口服的喹唑啉盐酸盐，具有潜在的抗肿瘤和放射增敏活性，抑制细胞EGFR和ErbB2自身磷酸化的IC50值分别为 7.4 和 9 nM。

Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.

Kinase inhibition: Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective Km for ATP (0.2 - 30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined using scintillation proximity assays with a retinoblastoma substrate and [γ-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting.

289499-45-2

C24H27Cl3FN5O3

558.86

CI-1033 dihydrochloride;PD-183805 dihydrochloride;Canertinib;卡奈替尼二盐酸盐

DMSO:55.9 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years